pharma-summit-gastro-summit-2018-keynote

4 / 6

N o v e m b e r 2 3 - 2 4 , 2 0 1 8 | B a n g k o k , T h a i l a n d
Note:
Page 17
Pharma Summit 2018 & Gastro Summit 2018 Asian Journal of Biomedical and Pharmaceutical Sciences | ISSN: 2249-622X | Volume 8
&
GLOBAL PHARMA SUMMIT
GASTROENTEROLOGY AND HEPATOLOGY
2nd International Conference on
Joint Event on
OF EXCELLENCE
IN INTERNATIONAL
MEETINGS
YEARS
Gopal Natesan, Asian J Biomed Pharmaceut Sci 2018, Volume 8 | DOI: 10.4066/2249-622X-C5-013
STUDIES ON 2-(4-METHOXY/METHYL)-
PHENYL – 3- SUBSTITUTED QUINAZOLIN-
4(3H)-ONE ANALOGS AS POTENTIAL
ANTIBACTERIAL AGENTS
T he development of antibiotic resistance in pathogenic microorganism is a
global health concern due to the emergence of multidrug resistant organ-
ism (MDRO). It is essential to synthesize novel antimicrobial agents to deal
with increased number of multidrug resistance organisms (MDRO) and lim-
ited antimicrobial agent. Literature survey showed that quinazolin-4(3H)-one
possess varied biological activities and 2nd and 3rd positions are the target for
substitution with other moieties. On the other hand, isatin and sulphanilamide
pharmacophore also exhibits wide range of pharmacological activities espe-
cially significant antibacterial activity though competitive inhibition of dihy-
dropteroate synthetase enzyme. Hence, it has thought worthwhile to study the
effects of these pharmacophoric moieties in one molecule with the base of
quinazolin-4(3H)-one nucleus for better the antibacterial activity. A series of
mannich bases, 2-(substituted phenyl)-3-[1-(substituted amino methyl)-2-ox-
oindolin-3-ylideneamino] quinazolin-4-(3H)-one derivatives and 2-(4’-sub-
stitutedphenyl)-3-[(N-2-oxoindolin-3-ylidene)-4”-sulphonamidophenyl]-
quinazolin-(3H)-one has synthesised. The title compound has synthesised
from the intermediate schiff bases which is prepared by reacting 2-(substitut-
ed phenyl)-4H-benzo[d][1,3]-oxazin-4-one with hydrazine hydrate/sulphanil-
amide followed by isatin and the required benzoxazinone derivate has been
prepared by reacting anthranilic acid with substituted benzoyl chloride. All
the synthesised compounds structures were characterised by using H1 Nu-
clear Magnetic Resonance Spectroscopy. The intermediate schiff base and
final mannich base compounds were evaluated for their antibacterial activity
against Staphylococcus aureus, Bacillus cereus, Escherichia coli and Pseudo-
monas aeruginosa at a concentration of 50 µg/mL and 100 µg/mL by agar well
diffusion method using Norfloxacin (50 µg/mL) as standard drug. From the
study, it has been observed that the sulphanilamide substituted derivatives
did not showed any inhibition against all the organism whereas amino substi-
tuted shciff and mannich base showed significant degree of inhibition. Finally,
it has been concluded that mannich base derivatives of amino substitution at
3rd position in quinazolinone nucleus exhibited a higher degree of inhibition
and also superior in its antibacterial activity against gram positive bacteria S.
aureus and B. cereus.
Keywords: Quinazolin-4(3H)-one, Sulphanilamide, Isatin, Mannich, Schiff
base, Antibacterial activity
Biography
Gopal Natesan has completed his Doctoral degree
(PhD) in Pharmaceutical Chemistry from Hamdard
University (Jamia Hamdard) New Delhi, India in
2000 and currently serving as Professor in Medici-
nal Chemistry, in MAHSA University, Malaysia. and
Director (Academic & Operation) MAHSA Prima
International College, MAHSA Group, Malaysia.
He has published >40 articles in indexed journals
and presented >80 papers in conferences and re-
ceived number of honors, recently received “Young
Scientist Award” in 2013 and “Edward Kennedy
Memorial Award” in 2017 for his high standards
of research excellence in Science and Technology.
He was invited speaker at international scientific
meetings and conferences and serves as reviewer
for several scientific international journals and also
as Editorial/Advisory board of various journals.
Gopal Natesan
MAHSA University, Malaysia